Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pralsetinib (Blu667) 是高效的、选择性的RET 抑制剂。它能够抑制 WT RET (IC50:0.4 nM),RET 突变体 V804L (IC50:0.3 nM),V804M (IC50:0.4 nM),M918T (IC50:0.4 nM) 和 CCDC6-RET (IC50:0.4 nM) 的融合。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 578 | 现货 | ||
2 mg | ¥ 778 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,830 | 现货 | ||
25 mg | ¥ 2,970 | 现货 | ||
50 mg | ¥ 4,460 | 现货 | ||
100 mg | ¥ 6,270 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,360 | 现货 |
产品描述 | Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion). |
靶点活性 | CCDC6-RET:0.4 nM, Wild type RET:0.4 nM, RET M918T:0.4 nM, RET V804M:0.4 nM, RET V804L:0.3 nM |
体外活性 | Pralsetinib demonstrates more than 10-fold increased potency over approved MKIs against oncogenic RET variants and resistance mutants. Pralsetinib demonstrates potent activity (IC50: 0.4 nM) against common oncogenic RET alterations, including RET M918T, an activating mutation found in MTC, as well as the CCDC6-RET fusion observed in PTC and NSCLC. Pralsetinib suppresses RET pathway signaling in a panel of RET-driven cell lines: LC2/ad (CCDC6-RET, NSCLC), MZ-CRC-1 (RET M918T, MTC), and TT (RET C634W, MTC). |
体内活性 | Pralsetinib potently inhibits the growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR-2. Pralsetinib shows dose-dependent activity against both KIF5B-RET Ba/F3 and KIF5B-RET V804L Ba/F3 allograft tumors with doses as low as 10 mg/kg twice daily. |
别名 | 普拉替尼, Blu667 |
分子量 | 533.6 |
分子式 | C27H32FN9O2 |
CAS No. | 2097132-94-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (178.04 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8741 mL | 9.3703 mL | 18.7406 mL | 46.8516 mL |
5 mM | 0.3748 mL | 1.8741 mL | 3.7481 mL | 9.3703 mL | |
10 mM | 0.1874 mL | 0.937 mL | 1.8741 mL | 4.6852 mL | |
20 mM | 0.0937 mL | 0.4685 mL | 0.937 mL | 2.3426 mL | |
50 mM | 0.0375 mL | 0.1874 mL | 0.3748 mL | 0.937 mL | |
100 mM | 0.0187 mL | 0.0937 mL | 0.1874 mL | 0.4685 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pralsetinib 2097132-94-8 Apoptosis Tyrosine Kinase/Adaptors c-RET Inhibitor BLU 667 BLU-667 普拉替尼 Blu667 inhibit RET inhibitor